4UIY

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(1,1-dioxo-1-thian-4-yl)- 5-methyl-4-oxo-7-3-(trifluoromethyl)phenyl-4H,5H-thieno-3,2-c- pyridine-2-carboximidamide

Summary for 4UIY

• Entry DOI: 10.2210/pdb4uiy/pdb
• Related: 4UIT 4UIU 4UIV 4UIW 4UIX 4UIZ
• Descriptor: BROMODOMAIN-CONTAINING PROTEIN 4, 1,2-ETHANEDIOL, N-[1,1-bis(oxidanylidene)thian-4-yl]-5-methyl-4-oxidanylidene-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide, ... (4 entities in total)
• Functional Keywords: transcription, inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Nucleus: O60885
• Total number of polymer chains: 1
• Total formula weight: 15769.11

Authors

Chung, C.,Theodoulou, N.T.,Bamborough, P.,Humphreys, P.G. (deposition date: 2015-04-03, release date: 2015-04-22, Last modification date: 2017-09-27)

• Primary citation: Theodoulou, N.H.,Bamborough, P.,Bannister, A.J.,Becher, I.,Bit, R.A.,Che, K.H.,Chung, C.,Dittmann, A.,Drewes, G.,Drewry, D.H.,Gordon, L.,Grandi, P.,Leveridge, M.,Lindon, M.,Michon, A.,Molnar, J.,Robson, S.C.,Tomkinson, N.C.O.,Kouzarides, T.,Prinjha, R.K.,Humphreys, P.G.; The Discovery of I-Brd9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.; J.Med.Chem., 59:1425-, 2016; PubMed: 25856009; DOI: 10.1021/ACS.JMEDCHEM.5B00256

Experimental method

X-RAY DIFFRACTION (1.3 Å)